Douche composition



Patented June 12, 1951 Lewing, Monson,vMass., assignors-to Tani-pap Incorporated, New York, N. ,Yl,. a.i.corp oration.

of Delaware No Drawing; Applicationt-April- 1 1949;

Serial .No. 85,026

12 Claims. (-01. un -58') invention relates to compositions adapted tovxbe used for treating the surfaces of mucousrmembranes of the human body and more-particu larly tr COII1I1OSitiOI1S that maybe advantageously incorporated in or used as a, douche. The press- 5w ent compositions may be solids adapted to-be dissolved in' waterto form a douche, or relatively concentrated solutions that must be diluted' be,- fore use, or solutions; that are sufficiently dilute so that they may be used without further dilution. This. application :is a continuation-in -partofgour prior applioation Serial No. 729,676; filed February 19, 1947, now abandoned.

A'sv pointedv outin' our; priorv application; it; is desirable that a douche for general douching purrl5 poses-have an effective.cleansinggactionv on the vaginal surfaces, that it be mildly astringent, and that it have an acidity approximatingsthat ofthe normal vagina, e2, arpI-I between 3.0: and;- 6:0? and preferably between 4.0: to 5.0; An alkalinel douche -is objectionable in that it interferes with the naturalreaction of the vaginal.- tract and: disturbs the development. of a normal bacterial 'flora -which-; is generally considered; -es-. sential to themaintenance oi a'rhealthy'condi; tion. Hence -'it is important that thelcomposition" used inpreparing thetdoucheibe capable. of l establishing-and maintaining :a desired aciditysof the douche: solution. Also it is important: that: the douche-solution" be free from components'which would destroy, for example, the-'so-caillediDod'er lein bacilli which are n'ormallyand desirably present in the vagina. It'is-ialso' desirablelthat the-components be non-toxic: and free from-irritating: and other "deleterious" properties" and that they 'bechemically and physically stable so that the composition may. be stored 'over a relativelylong period of time with'out'deteriorating:

It is accordingly an object of the present -inven-' tion to provide a mildly: acid, mildly astringent" 40.

and effectivelydetergent solution for treating-exposed or readily accessible mucous membrane surfaces. It is another objector theinventionto provide a'solid'composition'that is adapted'tobe' diss'olvedin a suitable medium such as'watr" to form a solution ofthis type that is especially adapted tobe used as a douche for cleansin vaginal surfaces. Itis still another object of the invention to provide a=dry,-' finely divided solid composition of this character that when dissolved in water forms a clear solution and iscapable of establishing and"; maintaining a d' esired acidity; i. e:, a pI-I'ofthe'order'of.410to 520'. It'ii's a further object of theiinvention to pro'-' yide a douche" solution ofthisityp'e' that. is free from.- componentswhichwould destroythe Doder ,1 lein bacillinormallyv present inthe vagina: It, is% a stilljfurther objecteof the-dnvention to provide adouche that -is' non-toxic, completely free f rorn. irritating, and deleterious I components and that has a beneficial. efiect on" vaginal. surfaces which it; comes; 1 incontact. Other obj ect s of the invention will be; in: partobvious-w and-1m part 'pointdputhereafter. y

We have found thatithe objects ofthe present invention may be achievedyin:general-by provid ing a. composition-comprising; a non-toxic, water-v soluble astringentselected from thergroupr consisti-ng or aluminum-and zinc -saltssand; a wetting;

agent. that'is compatible withsthe astringent in water'solution. i) Although. certain of-thesalts of metals other than zic and aluminum exhibit-an astringent action,'-,- it has;v been found: that the zinc; and aluminum more particularly; the sulfates of {these metals; have an- ;astringent ac- T tion" that is especially,- favorable in compositionsof'tlie present type. In 'order to-provide an-efiectiveI cleansing. action, we: prefer-to v usea :wetting, agent, ii. e one oflthe-socalle d .s oapless detergents as? distinguishedffrom an ordinary soap; While soaps; are" efictive, cleansing agents} for thispurpo ejtlif'ey. ai'iobjectionable in that theyare normally alkalinandhencetendto alter the 1 normally acidicofiditibii. of? the. vagina Moreover; they IoSeTtheir effectiveness .when-incorpo ratedfirfacid solution and are incompatible with solutions ofizin'an'd aluminum/salts, that" is to say; th'eyarei precipitated 'byminc. and aluminum saltsiinacid'solfitfoiir We ave'rbundz that a doucheincorporating; a-- suitable astring' 'ntr'ahdfwetting agent. asdescribed hferea'fter'," pr ds ari' unusually? efiective clans- V ing of thejf gifialfsurfaces. Such}. surfaces nor-- mallyh aV-' aI mucou's layen which is substantiall'y' impermeable to 1 most" aqueous solutions: The astri gent? of; the present. douche. operates to coagulate or clotTtliisj-rnu'cous layer thus permittingf'the wetting; ag'fitttq reach: and cleanse theundl'lyifigsfirfacsf Hence the astringent and. wetting, agent cooperate to give a detergent actiofitl'i'atfc'ahilbfi b' abl'l'ivd With either. component'alofie I murder to. eventidestiuctionof the:Dode rleir'i'ibacillil the Wftih'gfaightflsedlin tl'le resanti COlfiDbsitiOfif is" pifi abfi'" nonermicidal; Irr'ourcopndin "applicationlserial"No; 85,025; filed Abrilil; 1949, it ,isppifiteaf 01 thatv th fsllit abunyorawetuns agentjrdrusiifi douche sosin ns:oftne'preseuttybe "caiii'b'dtrnii ed by" subjecting thewettingfl aeent to' a standard germicidal test against Staph. am'eus, as described for example in U. S. Food and Drug Administration Methods of Testing Antiseptics and Disinfectants in U. S. Department of Agricultures circular No. 198 (December 1931). Wetting agents which when tested according to this procedure in aqueous solution are found to be non-germicidal against Staph. aureus at a dilution of 1:200 are disclosed in our copending application as being suitable for use in a douche of the present type and such compounds are defined in that application as non-germicidal wetting agents. We have further found that a particular wetting agent, namely alkylated aryl polyether alcohol, which may be the product sold under the trade name Triton X--100, is exceptionally useful in compositions of the type disclosed in this and our copending application in that it may be used-"in relatively high concentrations without killing Doderlein bacilli. More particularly we have found that the critical killing dilution of the alkylated aryl polyether alcohol against Doderlein bacilli is about 1:1000 as compared with 1:30,000 for the sodium lorolsulfoacetate and loroalkyl metasodium sulfobenzoate disclosed in our copending application. Thus the alkylated aryl polyether alcohol of the present application may be used at substantially higher concentrations than the wetting agents disclosed in our copending application and hence the resulting solution has a substantially more effective cleansing action. Compositions including non-germicidal wetting agents as a class are claimed in our copending applications whereas the claims of the present application are specific to compositions incorporating the alkylated aryl polyether alcohol.

The relative proportions of astringent and wetting agents are determined in some measure by the concentration desired in the douche solution when ready for use. The compatibility of the wetting agent and astringent varies somewhat according to the particular astringent and wetting agents used. We have found that from this point of view zinc salts, particularly zinc sulfate, are to be preferred. Other zinc salts that may be used are the chloride and the acetate. In general, the quantity of astringent should be suificient to give the desired coagulating action and the quantity of wetting agent should be suflicient to give an effective cleansing action but should not be so great as to kill the Doderlein bacilli. The solid compositions of the present invention are preferably compounded in such manner that, when they are dissolved in water to the final dilution for use as a douche, the concentration of astringent is between 0.06 and 0.5% by weight of the solution and the quantity of wetting agent is between 0.00016% and 0.1% by weight of the solution. The quantity of wetting agent should not, of course, exceed that which can be dissolved without precipitation in a solution containing the astringent.

As pointed out above, it is desirable that the acidity of the solution be established and maintained at a value approximating that of the normal vagina. It has been found that when aluminum sulfate, ammonium alum, or potassium alum are used as astringents the desired acidity is usually produced by the aluminum salt itself, whereas When zinc salts are used it is desirable that a small quantity of an acid or acid salt be added to the composition to adjust the acidity to a pH between 3.0 and 6.0 and preferably to a value between 4.0 and 5.0. It has been found particularly desirable to adjust the acidity of the douche with a mixture of sodium citrate and sodium acid citrate that provides a buffering action which maintains the pH of the douche within the desired range. The desired acidity can also be obtained by using any of various common acids such as sulfuric, acetic, tartaric, citric, malic or lactic acid or acid salts of these acids.

In the case of a solution that is to come in contact with a permeable membrane such as that of the vaginal surface it is desirable that the solution be approximately isotonic or perhaps somewhat hypertonic, i. e., that it contain a sufiicient quantity of sodium chloride to produce a solution having a concentration equivalent to or somewhat greater than that of the normal body saline. Accordingly the compositions of the present invention preferably include a quantity of sodium chloride such that when they are dissolved in water to the desired final dilution they contain that sodium chloride concentration which will make them at least approximately isotonic.

Various agents other than those previously mentioned may also be included in the solid compositions and solutions of the present invention to accomplish special purposes. In some cases it is desirable to add a conditioning agent such as lactose which favors the growth of the Doderlein bacilli. Also aromatic compounds such as menthol, oil of peppermint and the like may be included to render the product more agreeable in use.

In order to point out more fully the nature of the present invention, there are given below certain specific examples of the invention and its application in practical use and also certain modifications and alternatives. However, it should be understood that these are not intended to be exhaustive or to be limiting of the invention. On the contrary, these illustrations and the explanations herein are given in order to acquaint others skilled in the art with this invention and the principles thereof and a suitable manner of its application in practical use so that others skilled in the art may be enabled to modify the invention and to adapt it and to apply it in numerous forms each as may be best suited to the requirements of a particular use.

The examples given below are of solid compositions that may be dissolved in water to form a douche. These compositions when dissolved in water to the extent of 12 gms. per quartof water yield douche solutions that are substantially inactive toward Doderlein bacilli. As indicated above the astringent content of the present douche solutions may vary from 0.06% to 0.5% by weight of the solution. However, not all of the following compositions can be used at all dilutions corresponding to the astringent range stated and still be inactive toward Doderlein bacilli. In order to avoid destruction of the Doderlein bacilli the following compositions should be used at dilutions such that the wetting agent concentration does not exceed about 1:1000.

Example 1 Alkylated aryl polyether alcohol (Triton Aromatics q. s. a. d.

ates-tea -E.'x:ample 2 I Alkyla'ted aryl polyether alcohol (Triton X-1'00)' g "0.151 Zinc sulfate monohydrate 10.3 Lactose USP 10.0 Sodium citrate USP 8.0 Monosodium citrate 2.5 Color and aromatics q.:s. 'a.';d. Sodium chloride USP 68.4

Example 3 I Alkylated -aryl polyether alcohdlKTriton Alum exsiccated 7.6 Lactose USP 12-.0 Sodium citrate USP L 17.5 Citric :acid anhydrous USP F. 1.75 Color and aromatics q. s. a. d. Sodium chloride USP 60.4

Example .4

Alkylated aryl polyether alcohol (Triton .X100) 00113 Zinc sulfate monohydrate .1013 Lactose ,USP ;15.0 Sodium citrate USP 110.0 Tartaric acid USP -f. 1.75 Color and aromatics q. s. a. d. Sodium-chloride USP :623

Example 5 Alkylated aryl polyether alcohol (Triton X--100) 7.5 Zinc sulfate monohydrate 10.3 Lactose USP 10.0 Sodium citrate USP L .8. 0 Monosodium citrate 2.5 Color and aromatics q. s. a. d. Sodium chloride USP 61.4

Example 6 Alkylated aryl polyether alcohol (Triton X-100) Zinc sulfate monohydrate 5.0 Lactose USP 10.0 Sodium citrate USP 8.0 Monosodium citrate 2.5 Color and aromatics q. s. a. d. Sodium chloride USP 73.7

Example 7 Alkylated aryl polyether alcohol (Triton X--l00) Zinc sulfate monohydrate 39. Sodium citrate USP 8.0 Monosodium citrate 2.5 Color and aromatics q. s. a. (1. Sodium chloride USP 49.7

Example 8 Alkylated aryl polyether alcohol (Triton Xl00) 9.3 Zinc sulfate monohydrate 5.0 Lactose USP 12.3 Sodium citrate USP 8.0 Monosodium citrate 3.7

Color and aromatics q. s. a. d. Sodium chloride USP 60.5

From the foregoing examples and descriptions, it is apparent that the compositions of the present invention may be used to provide a douche that is non-toxic, free from irritating and deleterious components and has a beneficial effect on vaginal and other mucous membranes with which it comes in contact. As previously stated,

the present vcompositionsmaybe made up in the are i-insoluble in water and should dissolve ,com; pletely in water to form ,a clear solution. The;

acidity of the solutions prepared in accordance with present invention is established and maintained at pH .410 to 5.0 and there is thus no tendency for the solution to alter the-normal vaginal acidity. 'The astringent and wetting agent cooperate in the manner previously described to penetrate the thickened mucous masses and thoroughly cleanse the surfaces of the vagina. The compositions are chemically and physically stable and may, if necessary, be stored over long periods .of time without deterioration.

Since .many embodiments -;might be :made of the present invention and since many changes might be made in the embodiment disclosed herein, it is to be understood that the foregoing description is to be interpreted as illustrative only and not in a limiting sense.

Weclaim:

1. .A compositionofmatter adapted to be used in a douche, said composition comprising a nontoxic, water-soluble astringent selected from the group consisting of aluminum and zinc salts and aavetting agent which is an alkylated aryl polyether alcohol.

2. A composition adapted to .be used in .a

douche, said composition comprisinga non-toxic, water-soluble :zinc salt as an astringent and ran alkylated aryl polyether alcohol as a wetting agent. 7

. 3. .A composition adapted to Ibe -.used ,in ;.a douche, said composition comprising a non-toxic Water-soluble aluminum salt as an astringent and an alkylated aryl polyether alcohol as a wetting agent.

4. A composition adapted to be dissolved in water and used as a douche, said composition being a dry, finely divided solid comprising a nontoxic Water-soluble astringent selected from the group consisting of aluminum and zinc salts and an alkylated aryl polyether alcohol as a Wetting agent.

5. A composition adapted to be dissolved in Water and used as a douche, said composition being a dry, finely divided solid comprising a nontoxic water-soluble astringent selected from the group consisting of aluminum and zinc salts, an alkylated aryl polyether alcohol as a wetting agent and a quantity of an acidic substance sufficient to give said douche a pH of about 4.0 to 5.0.

6. A composition adapted to be dissolved in Water and used as a douche, said composition being a dry, finely divided solid comprising a nontoxic Water-soluble astringent selected from the group consisting of aluminum and zinc salts, an alkylated aryl polyether alcohol as a Wetting agent, a quantity of sodium chloride'sufficient to cause said douche solution to be approximately isotonic and a quantity of an acidic substance sufficient to give said douche solution a pH of about 4.0 to 5.0.

7. A composition adapted to be dissolved in Water and used as a douche, said composition being a dry, finely divided solid comprising a non-toxic water-soluble astringent selected from the group consisting of aluminum and zinc salts, an alkylated aryl polyether alcohol as a wetting agent, a conditioning agent which is lactose and a quantity of an acidic substance sufficient to 7. give said douche solution a pH of about 4.0 to 5.0.

8. A composition adapted to be dissolved in water and used as a douche, said composition being a dry, finely divided solid comprising zinc sulfate as an astringent, a minor proportion of an alkylated aryl polyether alcohol as a wetting agent and a quantity of an acidic substance sufficient to give said douche solution a pH of about 4.0 to 5.0.

9. A douche comprising a Water solution of a non-toxic astringent selected from the group consisting of aluminum and zinc salts, an alkylated aryl polyether alcohol as a wetting agent and a quantity of an acidic substance sufiicient to give said douche solution a pH of about 4.0 to 5.0, the concentration of said Wetting agent in said solution being less than 1:1000.

10. A douche comprising a Water solution of zinc sulfate as an astringent, an alkylated aryl polyether alcohol as a wetting agent and a quantity of an acidic substance sufficient to give said douche solution a pH of about 4.0 to 5.0, the concentration of said Wetting agent in said solution being less than 1 1000.

11. A composition adapted to be dissolved in water and used as a douche, said composition being a dry, finely divided solid comprising a non-toxic water-soluble astringent selected from the group consisting of aluminum and zinc salts, an alkylated aryl polyether alcohol as a Wetting agent and an acid bufler to maintain the pH of said solution at about 4.0 to 5.0.

12. A composition adapted to be dissolved in water and used as a douche, said composition being a dry, finely divided solid comprising a non-toxic Water-soluble astringent selected from the group consisting of aluminum and zinc salts,

an alkylated aryl polyether alcohol as a wetting agent and a quantity of a sodium citrate-sodium acid citrate buffer to maintain the pH of said solution at about 4.0 to 5.0.

JOHN H. WRIGHT. ALBERT W. LEWTING.

REFERENCES CITED The following references are of record in the file of this patent:

UNITED STATES PATENTS Number Name Date 2,114,370 Bickenheuser Apr. 19,1938 2,303,932 Guild Dec. 1, 1942 2,374,754 Kreidl et a1 May 1, 1945 2,436,184 Stillman Feb. 17, 1948 2,467,884 Elias Apr. 19, 1949' OTHER REFERENCES Novak: Urol. and Cut. Review, vol. 50, page (1946).

Karnaky: Southern Medical J., vol. 30, Jan. 1937, pages 69-70.

Harry: Manufacturing Chemist, Nov. 1940, 

1. A COMPOSITION OF MATTER ADAPTED TO BE USED IN A DOUCHE, SAID COMPOSITION COMPRISING A NONTOXIC, WATER-SOLUBLE ASTRINGENT SELECTED FROM THE GROUP CONSISTING OF ALUMINUM AND ZINC SALTS AND A WETTING AGENT WHICH IS AN ALKYLATED ARYL POLYETHER ALCOHOL. 